Assay Detail
Binding
CHEMBL666465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to the cloned human corticotropin releasing factor receptor 1
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.20 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333735 | — | — | 1 | 9.14 |
| CHEMBL295563 | — | — | 1 | 8.96 |
| CHEMBL413756 | — | — | 1 | 8.89 |
| CHEMBL65078 | — | — | 1 | 8.89 |
| CHEMBL333903 | — | — | 1 | 8.80 |
| CHEMBL121286 | — | — | 1 | 8.72 |
| CHEMBL332101 | — | — | 1 | 8.62 |
| CHEMBL120823 | — | — | 1 | 8.62 |
| CHEMBL333713 | — | — | 1 | 8.59 |
| CHEMBL121896 | — | — | 1 | 8.47 |
| CHEMBL331539 | — | — | 1 | 8.46 |
| CHEMBL263492 | — | — | 1 | 8.44 |
| CHEMBL334237 | — | — | 1 | 8.41 |
| CHEMBL122960 | — | — | 1 | 8.07 |
| CHEMBL330954 | — | — | 1 | 7.96 |
| CHEMBL333880 | — | — | 1 | 7.82 |
| CHEMBL121183 | — | — | 1 | 7.62 |
| CHEMBL121301 | — | — | 1 | 7.54 |
| CHEMBL123197 | — | — | 1 | 7.37 |
| CHEMBL121614 | — | — | 1 | 7.16 |
| CHEMBL121116 | — | — | 1 | 7.00 |
| CHEMBL123306 | — | — | 1 | 6.82 |
| CHEMBL122774 | — | — | 1 | - |
| CHEMBL332288 | — | — | 1 | - |
| CHEMBL332605 | — | — | 1 | - |
| CHEMBL332369 | — | — | 1 | - |
| CHEMBL122988 | — | — | 1 | - |
| CHEMBL334239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333735 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL295563 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL413756 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL65078 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL333903 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL121286 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL332101 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL120823 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL333713 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL121896 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL331539 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL263492 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL334237 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL122960 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL330954 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL333880 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL121183 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL121301 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL123197 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL121614 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL121116 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL123306 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL122774 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL332288 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL332605 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL332369 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL122988 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL334239 | — | Ki | > | 10000.0 | nM | - |